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PMC9145791
core_pubmed_pmc
A Pharmacometric Model to Predict Chemotherapy-Induced Myelosuppression and Associated Risk Factors in Non-Small Cell Lung Cancer
A Pharmacometric Model to Predict Chemotherapy-Induced Myelosuppression and Associated Risk Factors in Non-Small Cell Lung Cancer Abstract Chemotherapy often induces severe neutropenia due to the myelosuppressive effect. While predictive pharmacokinetic (PK)/pharmacodynamic (PD) models of absolute neutrophil count (ANC...
PMC6135786
core_pubmed_pmc
Fingerprints of CNS drug effects: a plasma neuroendocrine reflection of D 2 receptor activation using multi‐biomarker pharmacokinetic/pharmacodynamic modelling
Fingerprints of CNS drug effects: a plasma neuroendocrine reflection of D 2 receptor activation using multi‐biomarker pharmacokinetic/pharmacodynamic modelling Abstract Abstract Background and Purpose Because biological systems behave as networks, multi‐biomarker approaches increasingly replace single biomarker approac...
PMC10421770
core_pubmed_pmc
Preclinical Considerations for Long-acting Delivery of Tenofovir Alafenamide from Subdermal Implants for HIV Pre-exposure Prophylaxis
Preclinical Considerations for Long-acting Delivery of Tenofovir Alafenamide from Subdermal Implants for HIV Pre-exposure Prophylaxis Abstract Abstract Purpose Long-acting formulations of the potent antiretroviral prodrug tenofovir alafenamide (TAF) hold potential as biomedical HIV prevention modalities. Here, we prese...
PMC12256573
core_pubmed_pmc
Development and Verification of a Physiologically Based Pharmacokinetic Model of Furmonertinib and Its Main Metabolite for Drug–Drug Interaction Predictions
Development and Verification of a Physiologically Based Pharmacokinetic Model of Furmonertinib and Its Main Metabolite for Drug–Drug Interaction Predictions Abstract ABSTRACT Furmonertinib demonstrated potent efficacy as a newly developed tyrosine kinase inhibitor for the treatment of patients with epidermal growth fac...
PMC3528484
core_pubmed_pmc
A novel model-based approach for dose determination of glycopyrronium bromide in COPD
A novel model-based approach for dose determination of glycopyrronium bromide in COPD Abstract Background Glycopyrronium bromide (NVA237) is an inhaled long-acting muscarinic antagonist in development for treatment of COPD. This study compared the efficacy and safety of once-daily (OD) and twice-daily (BID) glycopyrron...
PMC12672812
core_pubmed_pmc
A randomised Phase 3 study comparing the efficacy and safety of proposed denosumab biosimilar RGB-14-P and reference denosumab in women with postmenopausal osteoporosis
A randomised Phase 3 study comparing the efficacy and safety of proposed denosumab biosimilar RGB-14-P and reference denosumab in women with postmenopausal osteoporosis Abstract Abstract Summary • In women with postmenopausal osteoporosis, proposed denosumab biosimilar RGB-14-P demonstrated equivalent efficacy and phar...
PMC12389043
core_pubmed_pmc
Repurposing Analysis of Nitroxoline (8-Hydroxy-5-nitroquinoline) as an Antichagasic Compound
Repurposing Analysis of Nitroxoline (8-Hydroxy-5-nitroquinoline) as an Antichagasic Compound Abstract Background/Objectives: Chagas disease, caused by the protozoan parasite Trypanosoma cruzi , remains a major neglected tropical disease, with over six million cases concentrated, primarily in Latin America. Despite deca...
PMC12158840
core_pubmed_pmc
PBPK Modeling to Support Bioavailability and Bioequivalence Assessment in Pediatric Populations
PBPK Modeling to Support Bioavailability and Bioequivalence Assessment in Pediatric Populations Abstract This report summarizes the proceedings for Session 3 of the one-day public workshop entitled “Advances in PBPK Modeling and its Regulatory Utility for Oral Drug Product Development” a jointly sponsored workshop by U...
PMC4474168
core_pubmed_pmc
Model-Based Assessment of Dosing Strategies in Children for Monoclonal Antibodies Exhibiting Target-Mediated Drug Disposition
Model-Based Assessment of Dosing Strategies in Children for Monoclonal Antibodies Exhibiting Target-Mediated Drug Disposition Abstract Abstract Body weight/body surface area–based and/or tiered fixed dosing strategies are widely utilized for monoclonal antibodies with linear clearance to scale adult clinical doses to c...
PMC9673920
core_pubmed_pmc
Clearance of therapeutic antibody glycoforms after subcutaneous and intravenous injection in a porcine model
Clearance of therapeutic antibody glycoforms after subcutaneous and intravenous injection in a porcine model Abstract ABSTRACT A relatively low clearance is one of the prominent favorable features of immunoglobulin G1-based therapeutic monoclonal antibodies (mAbs). Various studies have observed differential clearance o...
PMC9414337
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling to Describe the CYP2D6 Activity Score-Dependent Metabolism of Paroxetine, Atomoxetine and Risperidone
Physiologically Based Pharmacokinetic Modeling to Describe the CYP2D6 Activity Score-Dependent Metabolism of Paroxetine, Atomoxetine and Risperidone Abstract Abstract The cytochrome P450 2D6 ( CYP2D6 ) genotype is the single most important determinant of CYP2D6 activity as well as interindividual and interpopulation va...
PMC6916675
core_pubmed_pmc
First-In-Human Phase I Study Of A Dual mTOR Kinase And DNA-PK Inhibitor (CC-115) In Advanced Malignancy
First-In-Human Phase I Study Of A Dual mTOR Kinase And DNA-PK Inhibitor (CC-115) In Advanced Malignancy Abstract Abstract Purpose This first-in-human Phase I study investigated the safety, pharmacokinetics (PK), pharmacodynamic profile, and preliminary efficacy of CC-115, a dual inhibitor of mammalian target of rapamyc...
PMC12497770
core_pubmed_pmc
Clinical predictors and concomitant antiseizure medications effects on seizure control in relation to plasma cenobamate concentration: a multicenter retrospective study
Clinical predictors and concomitant antiseizure medications effects on seizure control in relation to plasma cenobamate concentration: a multicenter retrospective study Abstract Abstract Introduction Cenobamate (CNB) is a novel antiseizure medication (ASM) approved as an add-on therapy for drug-resistant focal onset se...
PMC9289112
core_pubmed_pmc
Population Pharmacokinetics and Dosing Regimen of Lithium in Chinese Patients With Bipolar Disorder
Population Pharmacokinetics and Dosing Regimen of Lithium in Chinese Patients With Bipolar Disorder Abstract Abstract Background : Lithium is an effective medication approved for the treatment of bipolar disorder (BD). It has a narrow therapeutic index (TI) and requires therapeutic drug monitoring. This study aimed to ...
PMC12827246
core_pubmed_pmc
Vitexin induces apoptosis and enhances daunorubicin efficacy in acute leukemia via modulation of the HIF-1α/Bcl-2/caspase-3 pathway
Vitexin induces apoptosis and enhances daunorubicin efficacy in acute leukemia via modulation of the HIF-1α/Bcl-2/caspase-3 pathway Abstract Acute leukemia is an aggressive hematologic malignancy with limited treatment success owing to drug resistance, severe adverse effects, and high costs. Vitexin, a natural compound...
PMC12249711
core_pubmed_pmc
Comprehensive Evaluation of 1H-Isoindole-1,3(2H)-Dione Derivatives: Pharmacokinetic Studies and Analgesic Potential in Various Pain Models
Comprehensive Evaluation of 1H-Isoindole-1,3(2H)-Dione Derivatives: Pharmacokinetic Studies and Analgesic Potential in Various Pain Models Abstract Abstract The study investigated the antinociceptive effects of four compounds (F1–F4) based on a 1H-isoindole-1,3(2H)-dione core, using various in vivo pain models—tonic (f...
PMC11350179
core_pubmed_pmc
Personalized dose selection for the first Waldenström macroglobulinemia patient on the PRECISE CURATE.AI trial
Personalized dose selection for the first Waldenström macroglobulinemia patient on the PRECISE CURATE.AI trial Abstract Abstract The digital revolution in healthcare, amplified by the COVID-19 pandemic and artificial intelligence (AI) advances, has led to a surge in the development of digital technologies. However, int...
PMC3337375
core_pubmed_pmc
Cross-simulation between two pharmacokinetic models for the target-controlled infusion of propofol
Cross-simulation between two pharmacokinetic models for the target-controlled infusion of propofol Abstract Abstract Background We investigated how one pharmacokinetic (PK) model differed in prediction of plasma (C p ) and effect-site concentration (C eff ) using a reproducing simulation of target-controlled infusion (...
PMC2791549
core_pubmed_pmc
Combined acetaminophen and ibuprofen for pain relief after oral surgery in adults: a randomized controlled trial
Combined acetaminophen and ibuprofen for pain relief after oral surgery in adults: a randomized controlled trial Abstract Abstract Background Acetaminophen is often used with a non-steriodal anti-inflammatory drug for acute pain. Hitherto, these drugs have had to be given separately, typically at different time interva...
PMC9264336
core_pubmed_pmc
Phase I/II study of streptozocin monotherapy in Japanese patients with unresectable or metastatic gastroenteropancreatic neuroendocrine tumors
Phase I/II study of streptozocin monotherapy in Japanese patients with unresectable or metastatic gastroenteropancreatic neuroendocrine tumors Abstract Abstract Background This phase I/II study was conducted to evaluate the efficacy, safety and pharmacokinetics of streptozocin (STZ) in Japanese patients with unresectab...
PMC11862786
core_pubmed_pmc
Population pharmacokinetics of tacrolimus whole blood and peripheral blood mononuclear cell concentrations in stable kidney‐transplanted patients
Population pharmacokinetics of tacrolimus whole blood and peripheral blood mononuclear cell concentrations in stable kidney‐transplanted patients Abstract Aim Therapeutic drug monitoring of tacrolimus based on whole blood drug concentrations is routinely performed. The concentration of tacrolimus in peripheral blood mo...
PMC12011033
core_pubmed_pmc
Investigating Remedial Strategies for Missed or Delayed Dose of Sertraline in Chinese Adolescent Patients with Depressive Disorders via Population Pharmacokinetics Modeling and Simulation Approaches
Investigating Remedial Strategies for Missed or Delayed Dose of Sertraline in Chinese Adolescent Patients with Depressive Disorders via Population Pharmacokinetics Modeling and Simulation Approaches Abstract Abstract Background Sertraline is a commonly used medication for adolescent patients with depression, and missed...
PMC12944453
core_pubmed_pmc
Development of Physiologically Based Pharmacokinetic (PBPK) Modeling
Development of Physiologically Based Pharmacokinetic (PBPK) Modeling Methods 2. Mechanistic Analysis of Pharmacokinetic Phenomena In Slavsky et al.’s publication, PBPK modeling is used to study drug–drug interactions (DDIs). Specifically, they research the induction of CYP2C metabolic enzymes, whose study with traditio...
PMC6861066
core_pubmed_pmc
Optimising systemic insecticide use to improve malaria control
Optimising systemic insecticide use to improve malaria control Abstract Background Long-lasting insecticidal nets and indoor residual sprays have significantly reduced the burden of malaria. However, several hurdles remain before elimination can be achieved: mosquito vectors have developed resistance to public health i...
PMC7151686
core_pubmed_pmc
Drug Dosing Considerations in Critically Ill Patients Receiving Continuous Renal Replacement Therapy
Drug Dosing Considerations in Critically Ill Patients Receiving Continuous Renal Replacement Therapy Abstract Abstract Acute kidney injury is very common in critically ill patients requiring renal replacement therapy. Despite the advancement in medicine, the mortality rate from septic shock can be as high as 60%. This ...
PMC11909909
core_pubmed_pmc
A single-dose, four-cycle, fully repetitive crossover bioequivalence of dabigatran etexilate in Chinese
A single-dose, four-cycle, fully repetitive crossover bioequivalence of dabigatran etexilate in Chinese Abstract Purpose Among healthy Chinese subjects, two capsules of dabigatran etexilate were tested for bioequivalence. Method Fifty healthy subjects were recruited for each of the fasting and postprandial trials in a ...
PMC3576170
core_pubmed_pmc
Clinical Trials of Potential Cognitive-Enhancing Drugs in Schizophrenia: What Have We Learned So Far?
Clinical Trials of Potential Cognitive-Enhancing Drugs in Schizophrenia: What Have We Learned So Far? Abstract In light of the number of studies conducted to examine the treatment of cognitive impairment associated with schizophrenia (CIAS), we critically reviewed recent CIAS trials. Trials were identified through sear...
PMC7262072
core_pubmed_pmc
Optimizing Hydroxychloroquine Dosing for Patients With COVID‐19: An Integrative Modeling Approach for Effective Drug Repurposing
Optimizing Hydroxychloroquine Dosing for Patients With COVID‐19: An Integrative Modeling Approach for Effective Drug Repurposing Abstract Hydroxychloroquine (HCQ) is a promising candidate for Coronavirus disease of 2019 (COVID‐19) treatment. The optimal dosing of HCQ is unknown. Our goal was to integrate historic and e...
PMC5278707
core_pubmed_pmc
Structure-Activity Relationships of a Series of Echinocandins and the Discovery of CD101, a Highly Stable and Soluble Echinocandin with Distinctive Pharmacokinetic Properties
Structure-Activity Relationships of a Series of Echinocandins and the Discovery of CD101, a Highly Stable and Soluble Echinocandin with Distinctive Pharmacokinetic Properties Abstract ABSTRACT Echinocandins are a first-line therapy for candidemia and invasive candidiasis. They are generally safe with few drug interacti...
PMC7192962
core_pubmed_pmc
Analysis of TRPA1 antagonist, A-967079, in plasma using high-performance liquid chromatography tandem mass-spectrometry
Analysis of TRPA1 antagonist, A-967079, in plasma using high-performance liquid chromatography tandem mass-spectrometry Abstract Abstract The noxious effects from exposure to toxic inhalation hazards (TIHs, such as isocyanates, chlorine, etc.) are known to be triggered by the activation of transient receptor potential ...
PMC8099444
core_pubmed_pmc
Approaches to handling missing or “problematic” pharmacology data: Pharmacokinetics
Approaches to handling missing or “problematic” pharmacology data: Pharmacokinetics Abstract Abstract Missing or erroneous information is a common problem in the analysis of pharmacokinetic (PK) data. This may present as missing or inaccurate dose level or dose time, drug concentrations below the analytical limit of qu...
PMC3406060
core_pubmed_pmc
Effect of Insulin Analogues on Insulin/IGF1 Hybrid Receptors: Increased Activation by Glargine but Not by Its Metabolites M1 and M2
Effect of Insulin Analogues on Insulin/IGF1 Hybrid Receptors: Increased Activation by Glargine but Not by Its Metabolites M1 and M2 Abstract Background In diabetic patients, the pharmacokinetics of injected human insulin does not permit optimal control of glycemia. Fast and slow acting insulin analogues have been devel...
PMC9326878
core_pubmed_pmc
Organic solute carrier 22 (SLC22) family: Potential for interactions with food, herbal/dietary supplements, endogenous compounds, and drugs
Organic solute carrier 22 (SLC22) family: Potential for interactions with food, herbal/dietary supplements, endogenous compounds, and drugs Abstract Abstract Many drugs, hormones, components of herbal medicines, environmental pesticides and toxins are Solute Carrier family 22 (SLC22) substrates. The last twenty years h...
PMC6537645
core_pubmed_pmc
Screening of Potential Phytocompounds From Euclea crispa (Thunb.) Leaves Targeting Human Epidermal Growth Factor Receptor 2 (HER2) Signaling Pathway
Screening of Potential Phytocompounds From Euclea crispa (Thunb.) Leaves Targeting Human Epidermal Growth Factor Receptor 2 (HER2) Signaling Pathway Abstract A BSTRACT Background: Overexpression of human epidermal growth factor receptor 2 (HER2) plays an important role in the development and progression in a variety of...
PMC12033005
core_pubmed_pmc
Clinical Pharmacology Overview of Tislelizumab in Patients With Advanced Tumors With a Focus on Racial Impact
Clinical Pharmacology Overview of Tislelizumab in Patients With Advanced Tumors With a Focus on Racial Impact Abstract ABSTRACT Tislelizumab, an anti‐programmed cell death protein‐1 monoclonal antibody, has demonstrated improved survival over the standard of care for multiple cancers. However, tislelizumab's effectiven...
PMC8590435
core_pubmed_pmc
Emergencies in obese patients: a narrative review
Emergencies in obese patients: a narrative review Abstract Obesity is associated to an increased risk of morbidity and mortality due to respiratory, cardiovascular, metabolic, and neoplastic diseases. The aim of this narrative review is to assess the physio-pathological characteristics of obese patients and how they in...
PMC11326704
core_pubmed_pmc
The use of quantitative clinical pharmacology approaches to support moxidectin dosing recommendations in lactation
The use of quantitative clinical pharmacology approaches to support moxidectin dosing recommendations in lactation Abstract Moxidectin is approved by the US Food and Drug Administration (US FDA) for the treatment of onchocerciasis (river-blindness) due to Onchocerca volvulus in patients aged 12 years and older. In onch...
PMC12753384
core_pubmed_pmc
Beyond monoclonal antibodies: constraints and the case for alternative PD-1/PD-L1-targeting formats
Beyond monoclonal antibodies: constraints and the case for alternative PD-1/PD-L1-targeting formats Abstract Abstract Programmed cell death protein 1 (PD-1)/programmed death-ligand 1 (PD-L1) blockade has reshaped immuno-oncology, with antibodies establishing benchmarks for survival and durability of response across mul...
PMC4726617
core_pubmed_pmc
Phenotyping of UGT1A1 Activity Using Raltegravir Predicts Pharmacokinetics and Toxicity of Irinotecan in FOLFIRI
Phenotyping of UGT1A1 Activity Using Raltegravir Predicts Pharmacokinetics and Toxicity of Irinotecan in FOLFIRI Abstract Background Irinotecan toxicity correlates with UGT1A1 activity. We explored whether phenotyping UGT1A1 using a probe approach works better than current genotyping methods. Methods Twenty-four Asian ...
PMC12579042
core_pubmed_pmc
Pharmacokinetic Characteristics of a Once-Weekly Combination Therapy of Insulin Icodec and Semaglutide Versus Its Separate Components in Chinese Individuals with Type 2 Diabetes
Pharmacokinetic Characteristics of a Once-Weekly Combination Therapy of Insulin Icodec and Semaglutide Versus Its Separate Components in Chinese Individuals with Type 2 Diabetes Abstract Introduction IcoSema is under development as a once-weekly injectable combination therapy of icodec (basal insulin) and semaglutide (...
PMC12688977
core_pubmed_pmc
GLP-1 receptor agonists and preconception planning: bridging the gap between obesity treatment and reproductive safety, a narrative review
GLP-1 receptor agonists and preconception planning: bridging the gap between obesity treatment and reproductive safety, a narrative review Abstract Abstract Background: Obesity and associated metabolic disorders such as type 2 diabetes mellitus and polycystic ovary syndrome are rising globally, contributing to infertil...
PMC11207518
core_pubmed_pmc
In Vitro Predictive Model for Intestinal Lymphatic Uptake: Exploration of Additional Enhancers and Inhibitors
In Vitro Predictive Model for Intestinal Lymphatic Uptake: Exploration of Additional Enhancers and Inhibitors Abstract Drug absorption via chylomicrons holds significant implications for both pharmacokinetics and pharmacodynamics. However, a mechanistic understanding of predicting in vivo intestinal lymphatic uptake re...
PMC8303964
core_pubmed_pmc
Influence of CYP2C9 Genetic Polymorphisms on the Pharmacokinetics of Losartan and Its Active Metabolite E-3174: A Systematic Review and Meta-Analysis
Influence of CYP2C9 Genetic Polymorphisms on the Pharmacokinetics of Losartan and Its Active Metabolite E-3174: A Systematic Review and Meta-Analysis Abstract Abstract This study aimed to investigate the influence of CYP2C9 genetic polymorphisms on the pharmacokinetics of losartan and its active metabolite, E-3174, thr...
PMC11225735
core_pubmed_pmc
Application of Monte Carlo simulation to optimise the dosage regimen of meropenem in patients with augmented renal clearance for Pseudomonas aeruginosa infection
Application of Monte Carlo simulation to optimise the dosage regimen of meropenem in patients with augmented renal clearance for Pseudomonas aeruginosa infection Abstract Abstract Objective To optimise the dosing regimen of meropenem for treating Pseudomonas aeruginosa (PA) infections in critically ill patients with au...
PMC7891412
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Safety of the Dual Orexin Receptor Antagonist Lemborexant: Findings From Single‐Dose and Multiple‐Ascending‐Dose Phase 1 Studies in Healthy Adults
Pharmacokinetics, Pharmacodynamics, and Safety of the Dual Orexin Receptor Antagonist Lemborexant: Findings From Single‐Dose and Multiple‐Ascending‐Dose Phase 1 Studies in Healthy Adults Abstract Abstract Lemborexant, a dual orexin receptor antagonist, is approved for the treatment of insomnia and is under investigatio...
PMC12274271
core_pubmed_pmc
Pharmacokinetics and Safety with Bioequivalence of Isosorbide Mononitrate Sustained-Release Tablets in Chinese Healthy Volunteers: Bioequivalence Study
Pharmacokinetics and Safety with Bioequivalence of Isosorbide Mononitrate Sustained-Release Tablets in Chinese Healthy Volunteers: Bioequivalence Study Abstract Purpose Isosorbide mononitrate was recommended for controlling anginal symptoms in patients with cardiovascular disease. We aimed to compare the pharmacokineti...
PMC7552307
core_pubmed_pmc
Oral Transmucosal Cannabidiol Oil Formulation as Part of a Multimodal Analgesic Regimen: Effects on Pain Relief and Quality of Life Improvement in Dogs Affected by Spontaneous Osteoarthritis
Oral Transmucosal Cannabidiol Oil Formulation as Part of a Multimodal Analgesic Regimen: Effects on Pain Relief and Quality of Life Improvement in Dogs Affected by Spontaneous Osteoarthritis Abstract Simple Summary Osteoarthritis is a progressive and degenerative condition that affects dog populations, causing pain. Th...
PMC4352449
core_pubmed_pmc
Effects of Green Tea Extracts on the Pharmacokinetics of Quetiapine in Rats
Effects of Green Tea Extracts on the Pharmacokinetics of Quetiapine in Rats Abstract Quetiapine is an atypical antipsychotic, used clinically in the treatment of schizophrenia, acute mania in bipolar disorders, and bipolar depression in adults. In this study, the effect of green tea extracts (GTE) on the pharmacokineti...
PMC12180087
core_pubmed_pmc
Leveraging In Silico and Artificial Intelligence Models to Advance Drug Disposition and Response Predictions Across the Lifespan
Leveraging In Silico and Artificial Intelligence Models to Advance Drug Disposition and Response Predictions Across the Lifespan Abstract ABSTRACT Incorporating inter‐individual differences in drug disposition and responses is essential for ensuring the safe and effective use of drugs in real‐world patients. Despite on...
PMC10143046
core_pubmed_pmc
Evaluation of a Cardiovascular Systems Model for Design and Analysis of Hemodynamic Safety Studies
Evaluation of a Cardiovascular Systems Model for Design and Analysis of Hemodynamic Safety Studies Abstract Abstract Early prediction, quantification and translation of cardiovascular hemodynamic drug effects is essential in pre-clinical drug development. In this study, a novel hemodynamic cardiovascular systems (CVS) ...
PMC11128422
core_pubmed_pmc
Efficacy, Safety, and Pharmacokinetics of AZD7442 (Tixagevimab/Cilgavimab) for Prevention of Symptomatic COVID-19: 15-Month Final Analysis of the PROVENT and STORM CHASER Trials
Efficacy, Safety, and Pharmacokinetics of AZD7442 (Tixagevimab/Cilgavimab) for Prevention of Symptomatic COVID-19: 15-Month Final Analysis of the PROVENT and STORM CHASER Trials Abstract Abstract Introduction The phase 3 PROVENT and STORM CHASER studies evaluated AZD7442 (tixagevimab/cilgavimab) for pre-exposure and po...
PMC5749565
core_pubmed_pmc
A retrospective examination of the US Food and Drug Administration’s clinical pharmacology reviews of oncology biologics for potential use of therapeutic drug monitoring
A retrospective examination of the US Food and Drug Administration’s clinical pharmacology reviews of oncology biologics for potential use of therapeutic drug monitoring Abstract Background Biologics have gained traction for use in oncology, but have demonstrate clinical variability for efficacy and safety. Therapeutic...
PMC11493839
core_pubmed_pmc
Rational quinidine dosage regimen for atrial fibrillation in Thoroughbred racehorses based on population pharmacokinetics
Rational quinidine dosage regimen for atrial fibrillation in Thoroughbred racehorses based on population pharmacokinetics Abstract Abstract Introduction Quinidine (QND) sulfate is an effective treatment for atrial fibrillation (AF) in horses, and several dosage regimens have been proposed to address its wide variabilit...
PMC3298374
core_pubmed_pmc
A Systems Biology Approach in Therapeutic Response Study for Different Dosing Regimens—a Modeling Study of Drug Effects on Tumor Growth using Hybrid Systems
A Systems Biology Approach in Therapeutic Response Study for Different Dosing Regimens—a Modeling Study of Drug Effects on Tumor Growth using Hybrid Systems Abstract Motivated by the frustration of translation of research advances in the molecular and cellular biology of cancer into treatment, this study calls for cros...
PMC10362170
core_pubmed_pmc
A point-of-care pharmacokinetic/pharmacodynamic trial in critically ill children: Study design and feasibility
A point-of-care pharmacokinetic/pharmacodynamic trial in critically ill children: Study design and feasibility Abstract Background High-quality, efficient, pharmacokinetic (PK), pharmacodynamic (PD), and safety studies in children are needed. Point-of-care trials in adults have facilitated clinical trial participation ...
PMC9054876
core_pubmed_pmc
Population pharmacokinetic analysis of tepotinib, an oral MET kinase inhibitor, including data from the VISION study
Population pharmacokinetic analysis of tepotinib, an oral MET kinase inhibitor, including data from the VISION study Abstract Purpose Tepotinib is a highly selective, potent, mesenchymal–epithelial transition factor (MET) inhibitor, approved for the treatment of non-small cell lung cancer (NSCLC) harboring MET exon 14 ...
PMC9101252
core_pubmed_pmc
In Silico and Experimental Investigation of the Biological Potential of Some Recently Developed Carprofen Derivatives
In Silico and Experimental Investigation of the Biological Potential of Some Recently Developed Carprofen Derivatives Abstract Abstract The efficient regioselective bromination and iodination of the nonsteroidal anti-inflammatory drug (NSAID) carprofen were achieved by using bromine and iodine monochloride in glacial a...
PMC9800957
core_pubmed_pmc
A self-guidance biological hybrid drug delivery system driven by anaerobes to inhibit the proliferation and metastasis of colon cancer
A self-guidance biological hybrid drug delivery system driven by anaerobes to inhibit the proliferation and metastasis of colon cancer Abstract Abstract Colorectal cancer is often accompanied by multiple organ metastasis. Anaerobic Bifidobacterium Infantis (BI) bacterial can selectively grow in hypoxic colorectal tumor...
PMC11993168
core_pubmed_pmc
Dataset on potential biochemical activities of Cylo phe-Ala-Asp-Gly-based compounds as Caspase 1 inhibitor
Dataset on potential biochemical activities of Cylo phe-Ala-Asp-Gly-based compounds as Caspase 1 inhibitor Abstract Abstract In this work, seven Cylo phe-Ala-Asp-Gly-based Compounds were optimized using Spartan’14 software. Series of software used in this work were Spartan 14, molecular operating environment (MOE), pad...
PMC5104463
core_pubmed_pmc
Predictors of Prolonged TB Treatment in a Dutch Outpatient Setting
Predictors of Prolonged TB Treatment in a Dutch Outpatient Setting Abstract Introduction Standard treatment duration for drug-susceptible tuberculosis (TB) treatment is 6 months. Treatment duration is often extended—and for various different reasons. The aim of this study was to determine the prevalence and to assess r...
PMC3296951
core_pubmed_pmc
Investigation of the Mechanism of Clearance of AMG 386, a Selective Angiopoietin-1/2 Neutralizing Peptibody, in Splenectomized, Nephrectomized, and FcRn Knockout Rodent Models
Investigation of the Mechanism of Clearance of AMG 386, a Selective Angiopoietin-1/2 Neutralizing Peptibody, in Splenectomized, Nephrectomized, and FcRn Knockout Rodent Models Abstract Abstract Purpose To investigate the mechanisms of clearance of AMG 386, an investigational recombinant peptide-Fc fusion protein (pepti...
PMC4876144
core_pubmed_pmc
Snapshot of the prescribing practice for the clopidogrel and esomeprazole coprescription and cost evaluation of the application guidelines
Snapshot of the prescribing practice for the clopidogrel and esomeprazole coprescription and cost evaluation of the application guidelines Abstract Abstract The antiplatelet clopidogrel and the proton pump inhibitor esomeprazole demonstrate a pharmacokinetic interaction through CYP 2C19 that could translate into clinic...
PMC9328431
core_pubmed_pmc
First‐in‐human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral doses of SAR247799, a selective G‐protein‐biased sphingosine‐1 phosphate receptor‐1 agonist for endothelial protection
First‐in‐human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral doses of SAR247799, a selective G‐protein‐biased sphingosine‐1 phosphate receptor‐1 agonist for endothelial protection Abstract Abstract Aims SAR247799 is a selective G‐protein‐biased sphingosine‐1 phosph...
PMC10339704
core_pubmed_pmc
Translation of the efficacy of antibody–drug conjugates from preclinical to clinical using a semimechanistic PK/PD model: A case study with RC88
Translation of the efficacy of antibody–drug conjugates from preclinical to clinical using a semimechanistic PK/PD model: A case study with RC88 Abstract Abstract Three semimechanistic pharmacokinetic/pharmacodynamic (PK/PD) models, Simeoni, Jumbe, and Hybrid, were used for the efficacy translation of RC88 from preclin...
PMC9299907
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics of the ADAMTS‐5 Inhibitor GLPG1972/S201086 in Healthy Volunteers and Participants With Osteoarthritis of the Knee or Hip
Safety, Pharmacokinetics, and Pharmacodynamics of the ADAMTS‐5 Inhibitor GLPG1972/S201086 in Healthy Volunteers and Participants With Osteoarthritis of the Knee or Hip Abstract Abstract GLPG1972/S201086 is a disintegrin and metalloproteinase with thrombospondin motif‐5 (ADAMTS‐5) inhibitor in development as an osteoart...
PMC10733441
core_pubmed_pmc
Pharmacodynamics of zoliflodacin plus doxycycline combination therapy against Neisseria gonorrhoeae in a gonococcal hollow-fiber infection model
Pharmacodynamics of zoliflodacin plus doxycycline combination therapy against Neisseria gonorrhoeae in a gonococcal hollow-fiber infection model Abstract Abstract Antimicrobial resistance in the sexually transmitted bacterium Neisseria gonorrhoeae is compromising the management and control of gonorrhea globally. Optimi...
PMC6206173
core_pubmed_pmc
Pharmacokinetics, Bioavailability, and Tissue Distribution Study of Angoroside C and Its Metabolite Ferulic Acid in Rat Using UPLC-MS/MS
Pharmacokinetics, Bioavailability, and Tissue Distribution Study of Angoroside C and Its Metabolite Ferulic Acid in Rat Using UPLC-MS/MS Abstract Abstract Angoroside C is a phenylpropanoid glycoside compound isolated from the dried root of Scrophularia ningpoensis Hemsl., which possesses the effects of preventing ventr...
PMC6271218
core_pubmed_pmc
Pharmacokinetics, Tissue Distribution and Excretion of Verticinone from F. hupehensis in Rats
Pharmacokinetics, Tissue Distribution and Excretion of Verticinone from F. hupehensis in Rats Abstract Abstract Verticinone, the main active component in F. hupehensis , exhibits potent antitussive and expectorant effects. Here, a LC-MS method was developed and applied to study the pharmacokinetics, tissue distribution...
PMC11968394
core_pubmed_pmc
The effect of deuterated PLK1 inhibitor on its safety and efficacy in vivo
The effect of deuterated PLK1 inhibitor on its safety and efficacy in vivo Abstract Background The FDA’s approval of deutetrabenazine, the first deuterium-labeled drug, demonstrated an improved safety profile compared to its non-deuterated counterpart, tetrabenazine. While Polo-like kinase 1 (PLK1) inhibitors have show...
PMC6449570
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic target attainment analyses to support intravenous and oral lefamulin dose selection for the treatment of patients with community-acquired bacterial pneumonia
Pharmacokinetic/pharmacodynamic target attainment analyses to support intravenous and oral lefamulin dose selection for the treatment of patients with community-acquired bacterial pneumonia Abstract Abstract Objectives Lefamulin is a semi-synthetic intravenous (iv) and oral pleuromutilin antibiotic active against commu...
PMC12083017
core_pubmed_pmc
Enhanced oral bioavailability of two Cistanche polysaccharides in acteoside: an in-depth analysis of intestinal flora, short-chain fatty acids, and pharmacokinetic regulation
Enhanced oral bioavailability of two Cistanche polysaccharides in acteoside: an in-depth analysis of intestinal flora, short-chain fatty acids, and pharmacokinetic regulation Abstract Abstract Introduction For centuries, Cistanche deserticola Y. C. Ma has been considered to have the effect of “tonifying the kidney and ...
PMC12575352
core_pubmed_pmc
QSAR-based physiologically based pharmacokinetic (PBPK) modeling for 34 fentanyl analogs: model validation, human pharmacokinetic prediction and abuse risk insights
QSAR-based physiologically based pharmacokinetic (PBPK) modeling for 34 fentanyl analogs: model validation, human pharmacokinetic prediction and abuse risk insights Abstract Abstract Introduction Fentanyl analogs, as emerging new psychoactive substances (NPS), pose a global public health threat due to widespread abuse,...
PMC10144684
core_pubmed_pmc
Toward Practical Integration of Omic and Imaging Data in Co-Clinical Trials
Toward Practical Integration of Omic and Imaging Data in Co-Clinical Trials Abstract Co-clinical trials are the concurrent or sequential evaluation of therapeutics in both patients clinically and patient-derived xenografts (PDX) pre-clinically, in a manner designed to match the pharmacokinetics and pharmacodynamics of ...
PMC8114026
core_pubmed_pmc
Anti–factor Xa activity assays of direct‐acting oral anticoagulants during clinical care: An observational study
Anti–factor Xa activity assays of direct‐acting oral anticoagulants during clinical care: An observational study Abstract Abstract Background Direct‐acting oral anticoagulants (DOACs) are increasingly used to prevent and treat thromboembolism. Although measurement of DOAC concentrations is not currently recommended as ...
PMC9977486
core_pubmed_pmc
Impact of Fasting Status and Circadian Variation on the Pharmacokinetics of Mycophenolate Mofetil and the Glucuronide Metabolite in Renal Transplant Recipients
Impact of Fasting Status and Circadian Variation on the Pharmacokinetics of Mycophenolate Mofetil and the Glucuronide Metabolite in Renal Transplant Recipients Abstract Background. Mycophenolate mofetil (MMF) is an immunosuppressive prodrug often used to prevent allograft rejection following solid organ transplantation...
PMC11397700
core_pubmed_pmc
Comprehensive Analysis of Berberis aristata DC. Bark Extracts: In Vitro and In Silico Evaluation of Bioaccessibility and Safety
Comprehensive Analysis of Berberis aristata DC. Bark Extracts: In Vitro and In Silico Evaluation of Bioaccessibility and Safety Abstract Abstract Berberine (BER) is an alkaloid found, together with other protoberberinoids (PROTBERs), in several species used in medicines and food supplements. While some herbal preparati...
PMC3398251
core_pubmed_pmc
Evaluation of onset of pain relief from micronized aspirin in a dental pain model
Evaluation of onset of pain relief from micronized aspirin in a dental pain model Abstract Abstract A new formulation of a micronized acetylsalicylic acid swallowable tablet with an effervescent component (FR-aspirin) was evaluated in two independent studies using the dental impaction pain model. These clinical studies...
PMC9795792
core_pubmed_pmc
Circulating miR-320a-3p and miR-483-5p level associated with pharmacokinetic–pharmacodynamic profiles of rivaroxaban
Circulating miR-320a-3p and miR-483-5p level associated with pharmacokinetic–pharmacodynamic profiles of rivaroxaban Abstract Abstract Background Novel biomarkers for personalizing anticoagulation remain undetermined. We aimed to investigate the association of plasma miRNAs with pharmacokinetic–pharmacodynamic (PK-PD) ...
PMC10320033
core_pubmed_pmc
Mechanism of new optimized Sheng-Mai-San Formula to regulate cardiomyocyte apoptosis through NMDAR pathway
Mechanism of new optimized Sheng-Mai-San Formula to regulate cardiomyocyte apoptosis through NMDAR pathway Abstract Abstract Background and objectives Ischemic heart failure (HF) has become a disease that seriously endangers people's life and health. As a herbal formula widely used in clinical practice, new optimized S...
PMC12334082
core_pubmed_pmc
Ultrasound-Targeted Nanobubbles Codelivering NKP-1339 and miR-142-5p for Synergistic Mitochondrial Immunogenic Cell Death and PD-L1 Inhibition in Cancer Therapy
Ultrasound-Targeted Nanobubbles Codelivering NKP-1339 and miR-142-5p for Synergistic Mitochondrial Immunogenic Cell Death and PD-L1 Inhibition in Cancer Therapy Abstract The combination of chemical immunotherapy and gene therapy holds great promise for malignant tumor treatment. Here, we developed an ultrasound-targete...
PMC8205002
core_pubmed_pmc
Bleomycin administered by laser-assisted drug delivery or intradermal needle-injection results in distinct biodistribution patterns in skin: in vivo investigations with mass spectrometry imaging
Bleomycin administered by laser-assisted drug delivery or intradermal needle-injection results in distinct biodistribution patterns in skin: in vivo investigations with mass spectrometry imaging Abstract Abstract Bleomycin (BLM) is being repositioned in dermato-oncology for intralesional and intra-tumoural use. Althoug...
PMC11035509
core_pubmed_pmc
Effect of Daridorexant on the Pharmacokinetics of Midazolam, and on the Pharmacokinetics and Pharmacodynamics of Warfarin in Healthy Male Subjects
Effect of Daridorexant on the Pharmacokinetics of Midazolam, and on the Pharmacokinetics and Pharmacodynamics of Warfarin in Healthy Male Subjects Abstract Background and Objectives Daridorexant, a dual orexin receptor antagonist was recently approved for the treatment of insomnia at doses up to 50 mg once per night. T...
PMC8929005
core_pubmed_pmc
In Silico Design of Dual-Binding Site Anti-Cholinesterase Phytochemical Heterodimers as Treatment Options for Alzheimer’s Disease
In Silico Design of Dual-Binding Site Anti-Cholinesterase Phytochemical Heterodimers as Treatment Options for Alzheimer’s Disease Abstract The number of patients with neurodegenerative diseases, particularly Alzheimer’s disease (AD), continues to grow yearly. Cholinesterase inhibitors (ChEIs) represent the first-line s...
PMC9291828
core_pubmed_pmc
Clinical Study of Single‐Stranded Oligonucleotide RO7062931 in Healthy Volunteers and Patients With Chronic Hepatitis B
Clinical Study of Single‐Stranded Oligonucleotide RO7062931 in Healthy Volunteers and Patients With Chronic Hepatitis B Abstract Abstract Background and Aims RO7062931 is an N‐acetylgalactosamine (GalNAc)‐conjugated single‐stranded locked nucleic acid oligonucleotide complementary to HBV RNA. GalNAc conjugation targets...
PMC3134946
core_pubmed_pmc
Pharmacokinetic Considerations for Digoxin in Older People
Pharmacokinetic Considerations for Digoxin in Older People Abstract Objective: This review aims to arm readers with a deep understanding of pharmacokinetics of digoxin. Data Sources: Pharmacology and pharmacokinetic references texts, and peer reviewed medical journal manuscripts indexed on Medline included based on cur...
PMC8204864
core_pubmed_pmc
Overall survival in metastatic melanoma correlates with pembrolizumab exposure and T cell exhaustion markers
Overall survival in metastatic melanoma correlates with pembrolizumab exposure and T cell exhaustion markers Abstract Abstract Trial data support an absence of an exposure–survival relationship for pembrolizumab. As these relationships remain unexamined in a real‐world setting, we determined them in metastatic melanoma...
PMC9035989
core_pubmed_pmc
Dosage Strategy of Linezolid According to the Trough Concentration Target and Renal Function in Chinese Critically Ill Patients
Dosage Strategy of Linezolid According to the Trough Concentration Target and Renal Function in Chinese Critically Ill Patients Abstract Background: Linezolid is associated with myelosuppression, which may cause failure in optimally treating bacterial infections. The study aimed to define the pharmacokinetic/toxicodyna...
PMC8917032
core_pubmed_pmc
A Randomised Study to Investigate the Nicotine Pharmacokinetics of Oral Nicotine Pouches and a Combustible Cigarette
A Randomised Study to Investigate the Nicotine Pharmacokinetics of Oral Nicotine Pouches and a Combustible Cigarette Abstract Abstract Background and Objectives Nicotine pouches (NPs) are a relatively new type of oral smokeless tobacco-free nicotine product. Currently, few data are available on the nicotine pharmacokin...
PMC7940400
core_pubmed_pmc
Programmable half-life and anti-tumour effects of bispecific T-cell engager-albumin fusions with tuned FcRn affinity
Programmable half-life and anti-tumour effects of bispecific T-cell engager-albumin fusions with tuned FcRn affinity Abstract Fc-less bispecific T-cell engagers have reached the immuno-oncology market but necessitate continual infusion due to rapid clearance from the circulation. This work introduces a programmable ser...
PMC4173331
core_pubmed_pmc
Admixture of clonidine and fentanyl to ropivacaine in epidural anesthesia for lower abdominal surgery
Admixture of clonidine and fentanyl to ropivacaine in epidural anesthesia for lower abdominal surgery Abstract Context and Background: Dose sparing action of one adjuvant for another in regional anesthesia. Aims and Objectives: To evaluate and compare the clonidine-ropivacaine combination with fentanyl-ropivacaine in e...
PMC2868991
core_pubmed_pmc
Explaining variability in ciclosporin exposure in adult kidney transplant recipients
Explaining variability in ciclosporin exposure in adult kidney transplant recipients Abstract Abstract Purpose Optimal ciclosporin A (CsA) exposure in kidney transplant recipients is difficult to attain because of variability in CsA pharmacokinetics. A better understanding of the variability in CsA exposure could be a ...
PMC12706402
core_pubmed_pmc
Model‐Informed Drug Development for Ligelizumab in Patients With Chronic Spontaneous Urticaria
Model‐Informed Drug Development for Ligelizumab in Patients With Chronic Spontaneous Urticaria Abstract ABSTRACT Model‐informed drug development (MIDD) has been increasingly applied to guide decision‐making, ameliorate efficiency, and enhance the likelihood of successful trials. The development of ligelizumab, a humani...
PMC12369981
core_pubmed_pmc
Long-Circulating Nanobody Confers Durable Prophylaxis against Severe Acute Respiratory Syndrome Coronavirus 2 Omicron Infection
Long-Circulating Nanobody Confers Durable Prophylaxis against Severe Acute Respiratory Syndrome Coronavirus 2 Omicron Infection Abstract Abstract Breakthrough infections in vaccinated population and continuous emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) variants make it imperative to devel...
PMC12737180
core_pubmed_pmc
Pharmacokinetics of CYP2C19- and CYP3A4-Metabolized Drugs in Cirrhosis Using a Whole-Body PBPK Approach
Pharmacokinetics of CYP2C19- and CYP3A4-Metabolized Drugs in Cirrhosis Using a Whole-Body PBPK Approach Abstract Abstract Background/Objectives : Cirrhosis significantly alters physiological function and drug metabolism, particularly for medications primarily metabolized by CYP2C19 and CYP3A4. This study aims to establ...
PMC6610665
core_pubmed_pmc
On the potential of in vitro organ-chip models to define temporal pharmacokinetic-pharmacodynamic relationships
On the potential of in vitro organ-chip models to define temporal pharmacokinetic-pharmacodynamic relationships Abstract Functional human-on-a-chip systems hold great promise to enable quantitative translation to in vivo outcomes. Here, we explored this concept using a pumpless heart only and heart:liver system to eval...
PMC10042892
core_pubmed_pmc
Justifying Ribociclib Dose in Patients with Advanced Breast Cancer with Renal Impairment Based on PK, Safety, and Efficacy Data: An Innovative Approach Integrating Data from a Dedicated Renal Impairment Study and Oncology Clinical Trials
Justifying Ribociclib Dose in Patients with Advanced Breast Cancer with Renal Impairment Based on PK, Safety, and Efficacy Data: An Innovative Approach Integrating Data from a Dedicated Renal Impairment Study and Oncology Clinical Trials Abstract Background and Objective Renal impairment is common in patients with canc...
PMC6037693
core_pubmed_pmc
Beyond the Blood:Brain Barrier: The Importance of Central Nervous System (CNS) Pharmacokinetics for the Treatment of CNS Tumors, Including Diffuse Intrinsic Pontine Glioma
Beyond the Blood:Brain Barrier: The Importance of Central Nervous System (CNS) Pharmacokinetics for the Treatment of CNS Tumors, Including Diffuse Intrinsic Pontine Glioma Abstract Over the past decade, we have made considerable progress in establishing diffuse intrinsic pontine glioma (DIPG) as a disease entity and de...
PMC10849900
core_pubmed_pmc
Developments in the Management of Growth Hormone Deficiency: Clinical Utility of Somapacitan
Developments in the Management of Growth Hormone Deficiency: Clinical Utility of Somapacitan Abstract Abstract Growth hormone (GH) replacement therapy for growth hormone deficiency (GHD) in children and adults has for over 25 years, until recently, been administered as daily injections. This daily treatment regimen oft...
PMC8131870
core_pubmed_pmc
Use of Protein Pegylation to Prolong the Antiviral Effect of IFN Against FMDV
Use of Protein Pegylation to Prolong the Antiviral Effect of IFN Against FMDV Abstract Abstract Interferons (IFNs) are considered the first line of defense against viral diseases. Due to their ability to modulate immune responses, they have become an attractive therapeutic option to control virus infections. In fact, l...
PMC8909008
core_pubmed_pmc
Evaluating Alternative Ramucirumab Doses as a Single Agent or with Paclitaxel in Second-Line Treatment of Locally Advanced or Metastatic Gastric/Gastroesophageal Junction Adenocarcinoma: Results from Two Randomized, Open-Label, Phase II Studies
Evaluating Alternative Ramucirumab Doses as a Single Agent or with Paclitaxel in Second-Line Treatment of Locally Advanced or Metastatic Gastric/Gastroesophageal Junction Adenocarcinoma: Results from Two Randomized, Open-Label, Phase II Studies Abstract Simple Summary Ramucirumab is indicated at a dosage of 8 mg/kg eve...